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41. 发明专利

HRP20100622T1 NEW CYCLOALKYLATED BENZOTHIADIAZINE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：HRP20100622T1
公开(公告)日：2010-12-31
申请号：HRP20100622
申请日：2010-11-17
申请人： SERVIER LAB
发明人： FRANCOTTE PIERRE , TULLIO PASCAL DE , PIROTTE BERNARD , DANOBER LAURENCE , LESTAGE PIERRE , CAIGNARD DANIEL-HENRI
IPC分类号： C07D285/28 , A61K31/549 , A61P25/00
摘要： Cycloalkyl benzothiadiazine derivatives (I) and their enantiomers, diastereoisomers, acid or base addition salts, are new. Cycloalkyl benzothiadiazine derivatives of formula (I) and their enantiomers, diastereoisomers, acid or base addition salts, are new. RCy : 3-8C cycloalkyl (optionally substituted by 1-6C alkyl (optionally substituted), halo, 1-6C alkoxy, hydroxy, or amino (optionally substituted by 1-6C alkyl)), or 1-6C-alkyl-(3-8C)cycloalkyl (optionally substituted on the cyclic part by 1-6C alkyl (optionally substituted by halo), 1-6C alkoxy, OH or amino (optionally substituted by 1-6C alkyl)); and R 1-R 4H, halo, nitro, CN, OH, thio, 1-6C alkyl (optionally substituted by halo), 1-6C alkoxy (optionally substituted by halo), 1-6C alkylthio, carboxy, 1-6C alkoxycarbonyl, 1-6C acyl, amino (optionally substituted by 1-6C alkyl or 1-6C acyl), aminocarbonyl (optionally substituted by 1-6C alkyl), aminosulfonyl (optionally substituted by 1-6C alkyl), or 1-6C alkylsulfonylamino. Provided that (I) is not 6-chloro-4-cyclohexyl-3,4-dihydro-7-sulfonamido-2H-1,2,4-benzothiadiazine-1,1-dioxide. Independent claims are included for: (1) the preparations of (I); (2) a composition comprising (I) in combination with inert, non-toxic vehicle; and (3) a benzo[1,2,4]thiadiazine-1,1-dioxide compound of formula (VI). [Image] [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Antiparkinsonian; Cerebroprotective; Anticonvulsant; Antialcoholic; Neuroleptic; Vasotropic. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor modulator. The AMPA receptor modulatory activity of (I) was tested in embryonic rat neurons, where the results were calculated as EC(2X) i.e. concentration of product that doubles the potential membrane induced by AMPA. The results showed that 6,7-dichloro-4-cyclopropyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxyde exhibited an EC(2X) value of 1 mu M.

42. 发明专利

RS51079B NOVI NAFTALENSKI DERIVATI, POSTUPAK NJIHOVE PROIZVODNJE I FARMACEUTSKE SMEŠE KOJE IH SADRŽE 未知
公开(公告)号：RS51079B
公开(公告)日：2010-10-31
申请号：RSP20090502
申请日：2007-06-29
申请人： SERVIER LAB
发明人： MILLAN MARK , BERTHELOT PASCAL , CAIGNARD DANIEL-HENRI , YOUS SAID , PERES BASILE , SABAOUNI AHMED , SPEDDING MICHAEL , DELAGRANGE PHILIPPE
IPC分类号： C07C233/18 , A61K31/165 , A61P9/00 , A61P15/00 , A61P25/00 , A61P35/00 , A61P37/02
摘要： Jedinjenje formule (I):ili N-[3-hidroksi-2-(7-metoksi-1-naftil)propil]propanamid, njegovi enantiomeri, kao i njihove adicione soli sa farmaceutski prihvatljivom bazom.Prijava sadrži još 6 zavisnih patentnih zahteva.

43. 发明专利

PT2147915E NOVOS DERIVADOS DE BENZOTIADIAZINAS CICLOALQUILADAS, PROCESSO PARA A SUA PREPARAÇÃO E AS COMPOSIÇÕES FARMACÊUTICAS QUE AS CONTENHAM 未知
公开(公告)号：PT2147915E
公开(公告)日：2010-10-13
申请号：PT09290547
申请日：2009-07-08
申请人： SERVIER LAB
发明人： LESTAGE PIERRE , PIROTTE BERNARD , CAIGNARD DANIEL-HENRI , FRANCOTTE PIERRE , TULLIO PASCAL DE , DANOBER LAURENCE
IPC分类号： C07D285/28 , A61K31/549 , A61P25/00

44. 发明专利

MA31577B1 NOUVEAUX DERIVES NAPHTALENIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知
公开(公告)号：MA31577B1
公开(公告)日：2010-08-02
申请号：MA32571
申请日：2010-02-01
申请人： SERVIER LAB
发明人： YOUS SAID , ETTAOUSSI MOHAMED , SABAOUNI AHMED , BERTHELOT PASCAL , SPEDDING MICHAEL , DELAGRANGE PHILIPPE , CAIGNARD DANIEL-HENRI , MILLAN MARK
IPC分类号： C07K251/48 , A61K31/165 , A61P25/00
摘要： COMPOSÉS DE FORMULE (I) : DANS LAQUELLE : R1 REPRÉSENTE UN ALKYLE, ALKÉNYLE, HALOGÉNOALKYLE, POLYHALOGÉNOALKYLE, CYCLOALKYLE, CYCLOALKYLALKYLE, ARYLE, ARYLALKYLE, HÉTÉROARYLE OU HÉTÉROARYLALKYLE, X REPRÉSENTE UN GROUPEMENT N-OR2 DANS LEQUEL R2 REPRÉSENTE UN ATOME D'HYDROGÈNE OU UN GROUPEMENT ALKYLE MÉDICAMENTS.

45. 发明专利

MX2010000001A DERIVADOS DE NAFTALENO NOVEDOSO, PROCESO PARA LA PREPARACION DE LOS MISMOS Y COMPOSICIONES FARMACEUTICAS QUE CONTIENEN LOS MISMOS. 未知
公开(公告)号：MX2010000001A
公开(公告)日：2010-04-21
申请号：MX2010000001
申请日：2008-07-01
申请人： SERVIER LAB
发明人： CAIGNARD DANIEL-HENRI , BERTHELOT PASCAL , DELAGRANGE PHILIPPE , MILLAN MARK , YOUS SAID , SABAOUNI AHMED , SPEDDING MICHAEL , ETTAOUSSI MOHAMED
IPC分类号： C07C233/18 , A61K31/165 , A61P25/00 , C07C233/60
摘要： Compuestos de f?rmula (I): en los cuales R1 es alquilo, alquenilo, haloalquilo, polihaloalquilo, cicloalquilo, cicloalquilalquilo, arilo, arilalquilo, heteroarilo, o heteroarilalquilo, y R2 es un ?tomo de fl?or o un grupo alquilo sustituido con uno o m?s ?tomos de fl?or. Medicamentos (ver f?rmula (I)).

46. 发明专利

AR070004A1 DERIVADOS NAFTALENICOS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：AR070004A1
公开(公告)日：2010-03-10
申请号：ARP080102855
申请日：2008-07-02
申请人： SERVIER LAB
发明人： SPEDDING MICHAEL , DELAGRANGE PHILIPPE , CAIGNARD DANIEL-HENRI , MILLAN MARK , SABAOUNI AHMED , BERTHELOT PASCAL , YOUS SAID , ETTAOUSSI MOHAMED
IPC分类号： C07C231/12 , A61K31/135 , A61P15/00 , A61P25/00 , A61P35/00 , C07C233/13
摘要： Reivindicacion 1: Compuesto de formula (1) sus enantiomeros, así como sus sales de adicion a una base aceptable farmacéuticamente. Reivindicacion 8: Composiciones farmacéuticas segun la reivindicacion 6 utiles para la fabricacion de medicamentos para el tratamiento de trastornos del sueno, estrés. ansiedad, depresion mayor o depresiones estacionales, patologías cardiovasculares, patologías del sistema digestivo, insomnios y fatigas debidos a diferencias horarias, esquizofrenia, ataques de pánico, melancolía, trastornos del apetito, obesidad, insomnio, trastornos psicoticos, epilepsia, diabetes, enfermedad de Parkinson demencia senil, diversos trastornos asociados al envejecimiento normal o patologico, migrana, pérdidas de memoria, enfermedad de Alzheimer, trastornos de la circulacion cerebral, así como en las disfunciones sexuales, como inhibidores de la ovulacion, inmunomoduladores y en el tratamiento de los cánceres.

47. 发明专利

DE602007002591D1 未知
公开(公告)号：DE602007002591D1
公开(公告)日：2009-11-12
申请号：DE602007002591
申请日：2007-06-29
申请人： SERVIER LAB
发明人： YOUS SAID , PERES BASILE , SABAOUNI AHMED , BERTHELOT PASCAL , SPEDDING MICHAEL , DELAGRANGE PHILIPPE , CAIGNARD DANIEL-HENRI , MILLAN MARK
IPC分类号： C07C233/18 , A61K31/165 , A61P9/00 , A61P15/00 , A61P25/00 , A61P35/00 , A61P37/02
摘要： N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide (I), its enantiomers and base addition salts, are new. N-[3-Hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide of formula (I), its enantiomers and base addition salts, are new. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Cerebroprotective; Contraceptive; Endocrine-Gen; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The ability of (I) to bind with melatonin was tested. The results showed that N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl] propanamide exhibited an inhibition constant value of 1.4 nM and 3.2 nM to bind with melatonin receptors MT 1 and MT 2, respectively.

48. 发明专利

EA012437B1 ПРОИЗВОДНЫЕ БЕНЗОКОНДЕНСИРОВАННЫХ ГЕТЕРОЦИКЛИЧЕСКИХ ОКСИМОВ, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И КОМБИНАЦИЯ И ИХ ПРИМЕНЕНИЕ 未知
公开(公告)号：EA012437B1
公开(公告)日：2009-10-30
申请号：EA200701476
申请日：2006-01-26
申请人： SERVIER LAB
发明人： HURTEVENT NATHALIE , L HELGOUAL CH JEAN-MARTIAL , CARATO PASCAL , LEBEGUE NICOLAS , LECLERC VERONIQUE , BERTHELOT PASCAL , DACQUET CATHERINE , KTORZA ALAIN , CAIGNARD DANIEL-HENRI
IPC分类号： C07D279/16 , A61K31/538 , A61K31/5415 , A61P3/06 , A61P3/10 , C07D265/36
摘要： Соединенияформулы (I)вкоторой X представляетсобойатомкислородаилиатомсеры, R, R, Rи Rимеютзначения, указанныев описании, Апредставляетсобойалкиленовуюцепь, какопределенов описании, иВ представляетсобойалкильнуюилиалкенильнуюгруппу, замещеннуюгруппойили R, илиВ представляетсобойгруппуили R. Лекарственныесредства.

49. 发明专利

MA30795B1 NOUVEAUX DERIVES INDOLIQUES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT. 未知
公开(公告)号：MA30795B1
公开(公告)日：2009-10-01
申请号：MA31791
申请日：2009-04-16
申请人： SERVIER LAB
发明人： MARCHAND PASCAL , BABONNEAU VINCENT , PIESSARD SYLVIE , DUFLOS MURIEL , BOUTIN JEAN ALBERT , AUDINOT VALERIE , DELAGRANGE PHILIPPE , CAIGNARD DANIEL-HENRI
IPC分类号： C07D209/42 , A61K31/404 , A61P1/00 , A61P15/00 , A61P25/00 , A61P35/00 , A61P9/00
摘要： COMPOSÉS DE FORMULE (I), DANS LAQUELLE R1 REPRÉSENTE UN GROUPEMENT ALKYLE, CYCLOALKYLE, OU CYCLOALKYLALKYLE; R2 REPRÉSENTE UN GROUPEMENT ALKYLE (C1-C6) LINÉAIRE OU RAMIFIÉ; ET N REPRÉSENTE 1 À 6, ET LEUR UTILISATION POUR TRAITER LES TROUBLES DU SYSTÈME MÉLATONINERGIQUE TELS QUE LES TROUBLES DU SOMMEIL, LE STRESS, L'ANXIÉTÉ, LES PATHOLOGIES CARDIOVASCULAIRES, ETC.

50. 发明专利

UA86801C2 КОМБИНАЦИЯ ГЕТЕРОЦИКЛИЧЕСКОГО СОЕДИНЕНИЯ И АНТИОКСИДАНТНОГО ВЕЩЕСТВА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, КОТОРАЯ ЕЕ СОДЕРЖИТ 未知
公开(公告)号：UA86801C2
公开(公告)日：2009-05-25
申请号：UAA200611437
申请日：2005-03-30
申请人： SERVIER LAB , CENTRE NAT RECH SCIENT
发明人： CASTEILLA LOUIS , PENICAUD LUC , BERTHELOT PASCAL , DACQUET CATHERINE , CAIGNARD DANIEL-HENRI
IPC分类号： A61K31/428 , A61K9/20 , A61K31/15 , A61P3/04
摘要： Комбинация, котораясодержитсоединение, котороеспособствуетметаболизмулипидови углеводов, иантиоксидантноевещество.

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